那那唑对血脂和脂蛋白代谢的影响。

C J Packard, J Shepherd
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引用次数: 0

摘要

达那唑是一种弱雄激素的杂环化合物,具有合成代谢特性,主要用于治疗子宫内膜异位症和其他妇科疾病。早期报告表明,该药物对血浆脂质(胆固醇和甘油三酯)水平几乎没有影响,但最近对达纳唑治疗后血浆脂质和脂蛋白代谢的更细微变化表示关注。治疗产生高密度脂蛋白(HDL)胆固醇的快速降低(特别是在假定的心脏保护HDL2亚段),同时导致致动脉粥样硬化的低密度脂蛋白(LDL)升高。这些明显不需要的作用与可能有益的减少致动脉粥样硬化脂蛋白(a)部分相平衡。达那唑诱导这些变化的机制尚不清楚,但可能与对肝脂肪酶、LDL受体和卵磷脂胆固醇酰基转移酶活性的影响有关。虽然认识到这些扰动可能带来的潜在危害是谨慎的,但只有在治疗时间延长(> 12个月)或对缺血性心脏病背景风险高的受试者进行治疗时才需要关注。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Action of danazol on plasma lipids and lipoprotein metabolism.

Danazol, a weakly androgenic, heterocyclic compound with anabolic properties, is used primarily in the treatment of endometriosis and other gynecological complaints. Early reports indicated that the drug had little effect on plasma lipid (cholesterol and triglyceride) levels but recently concern has been expressed over more subtle changes reported in plasma lipid and lipoprotein metabolism after danazol treatment. Therapy produces a rapid reduction in high density lipoprotein (HDL) cholesterol (particularly in the putatively cardioprotective HDL2 subfraction) coupled with a rise in the pro-atherogenic low density lipoprotein (LDL). These apparently unwanted actions are balanced against a possibly beneficial reduction in the atherogenic lipoprotein(a) fraction. The mechanism of these changes induced by danazol is unknown but probably relates to effects on hepatic lipase, LDL receptor and lecithin cholesterol acyl transferase activity. While it is prudent to recognize the potential detriment that may follow these perturbations, concern is only warranted where therapy is prolonged (> 12 months) or given to subjects with a high background risk of ischemic heart disease.

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